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1. 发明申请

WO2006047493A3 TASTE-MASKED PHARMACEUTICAL COMPOSITIONS WITH GASTROSOLUBLE PORE-FORMERS 审中-公开
标题翻译：具有气体成型剂的成型药物组合物
公开(公告)号：WO2006047493A3
公开(公告)日：2006-12-14
申请号：PCT/US2005038328
申请日：2005-10-21
申请人： EURAND PHARMACEUTICALS LTD , LAI JIN-WANG , VENKATESH GOPI M , QIAN KEN KANGYI
发明人： LAI JIN-WANG , VENKATESH GOPI M , QIAN KEN KANGYI
IPC分类号： A61K9/20 , A61K9/50
CPC分类号： A61K9/5078 , A61K9/0056 , A61K9/2081 , A61K9/501 , A61K9/5026 , A61K9/5047 , A61K31/135 , A61K31/4045 , A61K31/495
摘要： There is provided a method for preparing an orally disintegrating tablet (ODT) composition comprising microparticles of one or more taste-masked active pharmaceutical ingredient(s), rapidly-dispersing microgranules, and other optional, pharmaceutically acceptable excipients wherein the ODT disintegrates on contact with saliva in the buccal cavity forming a smooth, easy-to-swallow suspension. Furthermore, the microparticles (crystals, granules, beads or pellets containing the active), coated with a taste-masking membrane comprising a water-insoluble polymer and one or more gastrosoluble inorganic or organic pore-formers (practically insoluble in water and saliva, but soluble in an acidic buffer), exhibit acceptable taste-masking when placed in the oral cavity and provide rapid, substantially-complete release of the dose on entry into the stomach.
摘要翻译：提供了一种制备包含一种或多种掩味活性药物成分，快速分散微粒和其它任选的药学上可接受的赋形剂的微粒的口腔崩解片（ODT）组合物的方法，其中ODT与颊腔中的唾液形成平滑，易于吞咽的悬浮液。此外，涂覆有包含水不溶性聚合物和一种或多种胃溶性无机或有机成孔剂（实际上不溶于水和唾液，但几乎不溶于水和唾液，但是不溶于水）的掩味膜的微粒（晶体，颗粒，含有活性物质的颗粒或颗粒）可溶于酸性缓冲液），当放置在口腔中时显示出可接受的味道掩蔽，并且在进入胃中提供快速，基本上完全释放的剂量。

2. 发明申请

WO2006055142A8 TASTE-MASKED MULTIPARTICULATE PHARMACEUTICAL COMPOSITIONS COMPRISING A DRUG-CONTAINING CORE PARTICLE AND A SOLVENT-COACERVATED MEMBRANE 审中-公开
标题翻译：包含含药核心颗粒和溶剂型膜的烟味多药物药物组合物
公开(公告)号：WO2006055142A8
公开(公告)日：2006-11-16
申请号：PCT/US2005037084
申请日：2005-10-13
申请人： EURAND PHARMACEUTICALS LTD , LAI JIN-WANG , QIAN KEN , VENKATESH GOPI
发明人： LAI JIN-WANG , QIAN KEN , VENKATESH GOPI
IPC分类号： A61K9/16 , A61K9/20 , A61K9/48 , A61K31/4045 , A61K31/495
CPC分类号： A61K9/0056 , A61K9/1676 , A61K9/2077 , A61K31/4045 , A61K31/495
摘要： There is provided a method for preparing an orally disintegrating tablet (ODT) composition comprising microparticles of one or more taste-masked active pharmaceutical ingredients, rapidly-dispersing microgranules, and other optional, pharmaceutically acceptable excipients wherein the ODT disintegrates rapidly with saliva in the buccal cavity forming a smooth, easy-to-swallow suspension. Furthermore, the microparticles (crystals, granules, beads or pellets containing one or more actives) with a taste-masking membrane applied by a modified solvent coacervation process comprising a water-insoluble polymer and at least one gastrosoluble inorganic or organic pore-former, exhibit a pleasant taste when placed in the oral cavity and provide rapid, substantially-complete release of the dose on entry into the stomach.
摘要翻译：提供了一种制备包含一种或多种掩味活性药物成分，快速分散微粒和其它任选的药学上可接受的赋形剂的微粒的口腔崩解片（ODT）组合物的方法，其中ODT与颊内的唾液快速分解空腔形成平滑，易于吞咽的悬浮液。此外，通过包含水不溶性聚合物和至少一种胃溶性无机或有机成孔剂的改性溶剂凝聚方法施加的具有掩味膜的微粒（晶体，颗粒，含有一种或多种活性物质的珠粒或丸粒）当放置在口腔中时具有愉悦的味道并且在进入胃中提供快速，基本上完全释放的剂量。

3. 发明申请

WO2006055142A3 TASTE-MASKED MULTIPARTICULATE PHARMACEUTICAL COMPOSITIONS COMPRISING A DRUG-CONTAINING CORE PARTICLE ANS A SOLVENT-COACERVATED MEMBRANE 审中-公开
标题翻译：包含含药物颗粒的烟雾多药化学药物组合物ANS溶于溶剂的膜
公开(公告)号：WO2006055142A3
公开(公告)日：2006-07-20
申请号：PCT/US2005037084
申请日：2005-10-13
申请人： EURAND PHARMACEUTICALS LTD , LAI JIN-WANG , QIAN KEN , VENKATESH GOPI
发明人： LAI JIN-WANG , QIAN KEN , VENKATESH GOPI
IPC分类号： A61K9/16 , A61K9/20 , A61K9/48 , A61K31/4045 , A61K31/495
CPC分类号： A61K9/0056 , A61K9/1676 , A61K9/2077 , A61K31/4045 , A61K31/495
摘要： There is provided a method for preparing an orally disintegrating tablet (ODT) composition comprising microparticles of one or more taste-masked active pharmaceutical ingredients, rapidly-dispersing microgranules, and other optional, pharmaceutically acceptable excipients wherein the ODT disintegrates rapidly with saliva in the buccal cavity forming a smooth, easy-to-swallow suspension. Furthermore, the microparticles (crystals, granules, beads or pellets containing one or more actives) with a taste-masking membrane applied by a modified solvent coacervation process comprising a water-insoluble polymer and at least one gastrosoluble inorganic or organic pore-former, exhibit a pleasant taste when placed in the oral cavity and provide rapid, substantially-complete release of the dose on entry into the stomach.
摘要翻译：提供了一种制备口腔崩解片（ODT）组合物的方法，其包含一种或多种掩味活性药物成分的微粒，快速分散的微粒和其它任选的药学上可接受的赋形剂，其中ODT与颊内的唾液快速分解空腔形成平滑，易于吞咽的悬浮液。此外，通过包含水不溶性聚合物和至少一种胃溶性无机或有机成孔剂的改性溶剂凝聚方法施加的具有掩味膜的微粒（晶体，颗粒，含有一种或多种活性物质的珠粒或丸粒）当放置在口腔中时具有愉悦的味道并且在进入胃中提供快速，基本上完全释放的剂量。

4. 发明专利

IL291562D0 Corticosteroid containing orally disintegrating tablet compositions for eosinophilic esophagitis 未知
公开(公告)号：IL291562D0
公开(公告)日：2022-05-01
申请号：IL29156222
申请日：2022-03-21
申请人： ADARE PHARMACEUTICALS INC , GOSSELIN MICHAEL A , LAI JIN WANG , VENKATESH GOPI M
发明人： GOSSELIN MICHAEL A , LAI JIN-WANG , VENKATESH GOPI M
IPC分类号： A61K31/56 , A61K45/06 , A61P29/00 , B29C43/00
摘要： The present invention is directed to orally administered compositions of topically acting corticosteroids for the treatment of inflammation of the gastrointestinal tracts such as eosinophilic esophagitis. The present invention also provides a method for treating conditions associated with inflammation of the gastrointestinal tract in an individual. The method comprises administering to an individual in need thereof a pharmaceutical composition of the present invention as orally disintegrating tablets comprising a topically active corticosteroid adsorbed onto a pharmaceutically acceptable carrier such as silicified microcrystalline cellulose.

5. 发明专利

IL291562A Corticosteroid containing orally disintegrating tablet compositions for eosinophilic esophagitis 未知
公开(公告)号：IL291562A
公开(公告)日：2022-05-01
申请号：IL29156222
申请日：2022-03-21
申请人： ADARE PHARMACEUTICALS INC , GOSSELIN MICHAEL A , LAI JIN WANG , VENKATESH GOPI M
发明人： GOSSELIN MICHAEL A , LAI JIN-WANG , VENKATESH GOPI M
摘要： The present invention is directed to orally administered compositions of topically acting corticosteroids for the treatment of inflammation of the gastrointestinal tracts such as eosinophilic esophagitis. The present invention also provides a method for treating conditions associated with inflammation of the gastrointestinal tract in an individual. The method comprises administering to an individual in need thereof a pharmaceutical composition of the present invention as orally disintegrating tablets comprising a topically active corticosteroid adsorbed onto a pharmaceutically acceptable carrier such as silicified microcrystalline cellulose.

6. 发明申请

WO2012075455A3 RAPIDLY DISPERSING GRANULES, ORALLY DISINTEGRATING TABLETS AND METHODS 审中-公开
标题翻译：快速分散颗粒，ORALLY DISPATTING DISPATTING AND METHODS
公开(公告)号：WO2012075455A3
公开(公告)日：2013-06-27
申请号：PCT/US2011063172
申请日：2011-12-02
申请人： APTALIS PHARMATECH INC , VENKATESH GOPI M , SWAMINATHAN VIJAYA , LAI JIN-WANG , CLEVENGER JAMES M
发明人： VENKATESH GOPI M , SWAMINATHAN VIJAYA , LAI JIN-WANG , CLEVENGER JAMES M
IPC分类号： A61K9/14
CPC分类号： A61K9/2077 , A61K9/0056 , A61K9/167 , A61K9/2018 , A61K9/2027 , A61K9/205 , A61K9/2054 , A61K9/2095 , A61K31/137 , A61K31/167 , A61K31/351 , A61K31/4453 , A61K31/485 , A61K31/53 , A61K31/5513
摘要： This invention relates to rapidly dispersing microgranules comprising at least one sugar alcohol or saccharide, at least one super disintegrant, and a pharmaceutically acceptable additive with multi-functionality (e.g., starch acting as a binder, disintegrant, diluent/filler, glidant, etc) at a low level, which can be formed by not only eliminating a wet milling step but also avoiding an extensive dry milling step. Furthermore, such rapidly dispersing microgranules could also comprise a pharmaceutically active agent thereby providing for a pharmaceutical composition, or the rapidly dispersing microgranules thus produced are suitable for blending with a pharmaceutically active agent that is optionally taste-masked and/or controlled release coated microparticles to also provide for a pharmaceutical composition and the invention is also directed to a method for manufacturing such rapidly dispersing microgranules in a high useable yield, as well as orally disintegrating tablets comprising such rapidly dispersing microgranules. The rapidly dispersing microgranules are also free flowing.
摘要翻译：本发明涉及快速分散包含至少一种糖醇或糖，至少一种超级崩解剂和具有多官能度的药学上可接受的添加剂（例如，作为粘合剂的淀粉，崩解剂，稀释剂/填充剂，助流剂等）的微粒体，在低水平，其可以通过不仅消除湿磨步骤而且可以避免广泛的干磨步骤形成。此外，这种快速分散的微粒还可以包含药物活性剂，从而提供药物组合物，或由此制备的快速分散的微粒适合于与任选地掩蔽和/或控释的微粒的药物活性剂混合，还提供药物组合物，并且本发明还涉及以高可用产率制造这种快速分散的微粒的方法，以及包含这种快速分散的微粒的口腔崩解片剂。快速分散的微粒也是自由流动的。

7. 发明申请

WO2008027993A2 DRUG DELIVERY SYSTEMS COMPRISING SOLID SOLUTIONS OF WEAKLY BASIC DRUGS 审中-公开
标题翻译：包含弱碱性药物固体溶液的药物递送系统
公开(公告)号：WO2008027993A2
公开(公告)日：2008-03-06
申请号：PCT/US2007077153
申请日：2007-08-29
申请人： EURAND INC , VENKATESH GOPI , BOLTRI LUIGI , COLOMBO ITALO , LAI JIN-WANG , FLABIANI FLAVIO , MAPELLI LUIGI
发明人： VENKATESH GOPI , BOLTRI LUIGI , COLOMBO ITALO , LAI JIN-WANG , FLABIANI FLAVIO , MAPELLI LUIGI
IPC分类号： A61K31/4406 , A61K9/14 , A61K9/22 , A61K31/4422 , A61K31/454 , A61K31/5513 , A61K47/30 , A61K47/38
CPC分类号： A61K9/5026 , A61K9/5005 , A61K9/5042 , A61K9/5047 , A61K9/5078 , A61K9/5089 , A61K31/4406 , A61K31/4422 , A61K31/454 , A61K31/5513
摘要： The present invention is directed to pharmaceutical compositions and dosage forms comprising TPR beads, wherein said TPR beads comprise a solid dispersion of at least one active pharmaceutical ingredient in at least one solubility-enhancing polymer, and a TPR coating comprising a water insoluble polymer and an enteric polymer, wherein the active pharmaceutical ingredient comprises a weakly basic active pharmaceutical ingredient having a solubility of not more than 100 µg/mL at pH 6.8.
摘要翻译：本发明涉及包含TPR珠的药物组合物和剂型，其中所述TPR珠包含至少一种活性药物成分在至少一种溶解度增强聚合物中的固体分散体，和包含水不溶性聚合物和肠溶聚合物，其中活性药物成分包含在pH6.8时溶解度不超过100μg/ mL的弱碱性活性药物成分。

8. 发明申请

WO2010127345A2 ORALLY DISINTEGRATING TABLET COMPOSITIONS COMPRISING COMBINATIONS OF HIGH AND LOW-DOSE DRUGS 审中-公开
标题翻译：包含高剂量和低剂量组合的片剂组合物的ORALLY DISC
公开(公告)号：WO2010127345A2
公开(公告)日：2010-11-04
申请号：PCT/US2010033389
申请日：2010-05-03
申请人： EURAND INC , VENKATESH GOPI M , CLEVENGER JAMES , GOSSELLIN MICHAEL , LAI JIN-WANG
发明人： VENKATESH GOPI M , CLEVENGER JAMES , GOSSELLIN MICHAEL , LAI JIN-WANG
IPC分类号： A61K9/16
CPC分类号： A61K9/5047 , A61K9/2081 , A61K9/5073 , A61K9/5078 , A61K9/5084 , A61K31/00 , A61K31/192 , A61K31/196 , A61K31/40 , A61K31/405 , A61K31/407 , A61K31/415 , A61K31/4415 , A61K31/4468 , A61K31/485 , A61K31/5415 , A61K31/60 , A61K45/06 , A61K2300/00
摘要： The present invention is directed to pharmaceutical compositions comprising a plurality of taste-masked high-dose/low-dose drug-containing microparticles, dosage forms comprising such pharmaceutical compositions (such as an orally disintegrating tablet), and methods of making the pharmaceutical compositions and dosage forms of the present invention. Dosage forms comprising the pharmaceutical compositions of the present invention are improved homogeneous blends of high-dose and low-dose drugs which provide for more convenient and palatable administration of drug combinations, for example for treating pain, hyperglycemia, cardiovascular disease, and allergies.
摘要翻译：本发明涉及包含多个掩味的高剂量/低剂量药物的微粒的药物组合物，包含这种药物组合物（例如口腔崩解片剂）的剂型，以及制备该药物组合物的方法和本发明的剂型。包含本发明的药物组合物的剂型是改善的大剂量和低剂量药物的均匀共混物，其提供药物组合的更方便和可口的给药，例如用于治疗疼痛，高血糖症，心血管疾病和过敏症。

9. 发明申请

WO2007090082A3 DRUG DELIVERY SYSTEMS COMPRISING WEAKLY BASIC SELECTIVE SEROTONIN 5-HT3 BLOCKING AGENT AND ORGANIC ACIDS 审中-公开
标题翻译：包含弱碱性选择性丝氨酸5-HT3阻断剂和有机酸的药物递送系统
公开(公告)号：WO2007090082A3
公开(公告)日：2007-12-21
申请号：PCT/US2007061217
申请日：2007-01-29
申请人： EURAND INC , VENKATESH GOPI M , LAI JIN-WANG , VYAS NEHAL H
发明人： VENKATESH GOPI M , LAI JIN-WANG , VYAS NEHAL H
IPC分类号： A61K9/22
CPC分类号： A61K9/2077 , A61K9/0056 , A61K9/5073 , A61K9/5084 , A61K31/4178
摘要： A pharmaceutical dosage form such as a capsule, a conventional or orally disintegrating tablet capable of delivering a weakly basic, nitrogen (N)-containing selective serotonin 5- HT 3 blocking agent having a pKa in the range of from about 5 to 14 and a solubility of not more than about 200 µg/mL at pH 6.8 into the body in a sustained-released fashion, suitable for a once-daily dosing regimen, comprises at least one organic acid, which solubilizes said weakly basic selective serotonin 5-HT 3 blocking agent prior to releasing it into the hostile intestinal environment wherein the blocking agent is practically insoluble. The unit dosage form may be composed of a multitude of multicoated particulates (i.e., immediate-release beads, sustained-release beads and/or one or more timed, pulsatile- release bead populations) and is designed in such a way that the weakly basic blocking agent and the organic acid do not come into close contact during processing and/or storage thereby avoiding in-situ formation of acid addition compounds while ensuring that the acid is not depleted prior to completion of the drug release.
摘要翻译：一种药物剂型，例如胶囊，常规或口腔崩解片，其能够递送具有pKa范围的弱碱性，含氮（N）的选择性5-羟色胺5-羟色胺阻断剂约5至14，并且以pH 6.8的不超过约200μg/ mL的溶解度以持续释放的方式适应于每日一次的给药方案，包含至少一种有机酸，其溶解所述弱化碱性选择性5-羟色胺5-HT 3封闭剂，然后将其释放到敌对的肠道环境中，其中封闭剂几乎不溶。单位剂量形式可以由多种多重微粒（即即释丸，缓释珠和/或一个或多个定时，脉冲释放珠群）组成，并且以这样的方式设计：弱碱性封闭剂和有机酸在加工和/或储存期间不会紧密接触，从而避免了原位形成酸加成化合物，同时确保在药物释放完成之前酸不被耗尽。

10. 发明专利

CA2708152A1 ORALLY DISINTEGRATING TABLETS COMPRISING DIPHENHYDRAMINE 未知
公开(公告)号：CA2708152A1
公开(公告)日：2009-06-18
申请号：CA2708152
申请日：2008-12-09
申请人： EURAND INC , VENKATESH GOPI
发明人： LAI JIN-WANG , PERCEL PHILLIP , KRAMER CRAIG , VENKATESH GOPI
IPC分类号： A01N43/04 , A61K9/24
摘要： The compositions of the present invention comprise a therapeutically effective amount of particles consisting of diphenhydramine or pharmaceutically acceptable salts thereof, optionally in combination with another drug such as pseudoephedrine, or phenylephrine and hydrocodone, in combination with rapidly-dispersing microgranules comprising a disintegrant and a sugar alcohol and/or a saccharide. These compositions are useful in treating the symptoms of one or more diseases or conditions in which diphenhydramine (alone or in combination with one or two other drugs) is a therapeutically effective, e.g. allergic rhinitis, sinusitis, upper respiratory tract infections, motion sickness, Parkinson's disease, insomnia, the common cold, and nighttime pain management, particularly for subjects or patients with dysphagia, and people 'on the move'.

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